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信号转导和转录激活因子3(STAT3)的新型抑制剂:最新专利综述(2022年至今)

Novel inhibitors of STAT3: an updated patent review (2022-present).

作者信息

Bao Keting, Li Peiran, Gao Dingding

机构信息

School of Health Science and Nursing, Shanghai Sipo Polytechnic, Shanghai, China.

Innovation Research Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, China.

出版信息

Expert Opin Ther Pat. 2025 Jul;35(7):695-717. doi: 10.1080/13543776.2025.2494857. Epub 2025 Apr 22.

DOI:10.1080/13543776.2025.2494857
PMID:40238595
Abstract

INTRODUCTION

Signal transducer and activator of transcription 3 (STAT3), a member of the STAT protein family, serves as both a signal transducer and a transcription factor. Previous studies have highlighted its pivotal roles in regulating cell proliferation, differentiation, apoptosis, as well as immune and inflammatory responses. Consequently, targeting STAT3 has emerged as a promising therapeutic strategy for addressing related diseases.

AREAS COVERED

This review offers a comprehensive summary of the progress in discovering STAT3 inhibitors, with a focus on their structural diversity and structure-activity relationships as presented in patent literature from 2022 to the present.

EXPERT OPINION

Over the past decades, significant progress has transformed STAT3 into a target of interest for drug development. Despite these advances, no STAT3-targeting drugs have successfully progressed through late-phase clinical trials, largely due to challenges such as limited selectivity and undesirable side effects. These obstacles highlight the inherent complexity of developing safe and effective STAT3 inhibitors. Nevertheless, STAT3 remains a highly promising therapeutic target, and ongoing advancements in this field hold the potential to unlock novel strategies for addressing STAT3-related diseases.

摘要

引言

信号转导与转录激活因子3(STAT3)是STAT蛋白家族的成员,既是信号转导子又是转录因子。先前的研究突出了其在调节细胞增殖、分化、凋亡以及免疫和炎症反应中的关键作用。因此,靶向STAT3已成为治疗相关疾病的一种有前景的治疗策略。

涵盖领域

本综述全面总结了STAT3抑制剂发现方面的进展,重点关注2022年至今专利文献中呈现的其结构多样性和构效关系。

专家观点

在过去几十年中,显著进展使STAT3成为药物开发的一个有吸引力的靶点。尽管取得了这些进展,但尚无靶向STAT3的药物成功通过后期临床试验,这主要是由于选择性有限和不良副作用等挑战。这些障碍凸显了开发安全有效的STAT3抑制剂的内在复杂性。然而,STAT3仍然是一个非常有前景的治疗靶点,该领域的持续进展有可能解锁治疗STAT3相关疾病的新策略。

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